ペランパネル水和物

ペランパネル水和物 化学特性,用途語,生産方法

• 効能

  抗てんかん薬, AMPA受容体拮抗薬

• 商品名

  フィコンパ (エーザイ)

• 臨床応用

  Perampanel is a selective, non-competitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) antagonist approved for partial-onset seizures in patients with epilepsy. Perampanel was discovered and developed by Eisai.

• 合成

  A number of synthetic routes to perampanel have been reported and the process scale route is described herein.Bromination of commercial 2-methoxypyridine (120) gave 5-bromo-2-methoxypridine 121 in 86% yield (the scheme). Lithium halogen exchange was then accomplished by treating 121 with nbutyllithium followed by reaction with 2-benzenesulfonylpyridine (122) to provide bi-aryl 123 which was hydrolyzed under acidic conditions to give pyridine 124 in 60% overall yield. N-Arylation with triphenylboroxine (125) in the presence of copper acetate afforded N-aryl pyridine 126 in 91% yield. Pyridone 126 was reacted with N-bromosuccinimide to give bromopyridine 127 which was coupled with 2-(1,3,2-dioxaborinan-2-yl)benzonitrile (128) under palladium catalyzed conditions to give perampanel hydrate (XIX) in 86% yield after recrystallization from acetone/H2O.

  

ペランパネル水和物 生産企業

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